Bezafibrate (DB01393): A Comprehensive Pharmacological and Clinical Review

Section 1: Introduction

Bezafibrate is a well-established second-generation fibric acid derivative, classified as a lipid-modifying agent within the fibrate class of drugs.[1] Patented in 1971 and first approved for medical use in 1978, it has accumulated more than a quarter of a century of therapeutic experience in the management of dyslipidemia.[1] Its primary clinical application is as an adjunct to diet and other non-pharmacological measures for the treatment of various forms of hyperlipidemia, where it effectively reduces elevated levels of triglycerides and cholesterol while increasing high-density lipoprotein cholesterol (HDL-C).[3]

The most defining characteristic of Bezafibrate, which distinguishes it from other fibrates such as fenofibrate and gemfibrozil, is its unique and broad pharmacological profile as a pan-Peroxisome Proliferator-Activated Receptor (pan-PPAR) agonist.[1] While other fibrates act predominantly as selective agonists for the PPARα subtype, Bezafibrate binds to and activates all three PPAR isotypes—alpha (

PPARα), gamma (PPARγ), and delta (PPARδ)—at comparable and clinically relevant concentrations.[1] This balanced, pan-agonist activity confers a multifaceted mechanism of action that extends beyond simple lipid modulation. It allows Bezafibrate to influence a complex network of metabolic and cellular processes, including glucose homeostasis, inflammation, endothelial function, and fibrinogen metabolism.[6]